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    • 7. 发明申请
    • PALIPERIDONE OR A PHARMACEUTICALLY ACCEPTABLE SALT THEREOF SUBSTANTIALLY FREE OF IMPURITIES
    • 帕利哌酮或药物可接受的盐,大部分不含杂质
    • WO2011030224A3
    • 2011-03-17
    • PCT/IB2010/002568
    • 2010-09-10
    • ACTAVIS GROUP PTC EHFDIXIT, GirishKHILE, Anil, ShahajiPATEL, Jayesh, LaljibhaiPRADHAN, Nitin, Sharadchandra
    • DIXIT, GirishKHILE, Anil, ShahajiPATEL, Jayesh, LaljibhaiPRADHAN, Nitin, Sharadchandra
    • C07D471/04A61K31/519A61P25/00
    • Provided herein are impurities of paliperidone, 3-[2-[4-[l-(4-fruoro-2-hydroxyphenyl) methanoyl]piperidinyl-l-yl]ethyl]-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[l,2-a]pyrimidin-4- one (methanoyl impurity), 3-[2-[4-(6-fluoro-l,2-benzisoxazol-3-yl)-l-piperidinyl]ethyl]-2- methyl-4H-pyrido[l,2-a]pyrimidin-4-one (dehydroxy impurity) and 3-[2-[4-(6-fluoro-l,2- benzisoxazol-3-yl)-l-piperidinyl]ethyl]-2-methyl-7,8-dihydro-6H-pyrido[l,2-a]pyrimidin- 4,9-dione (9-keto impurity), and processes for preparing and isolating thereof. Provided further herein is a highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9-keto impurities, process for the preparation thereof, and pharmaceutical compositions comprising highly pure paliperidone or a pharmaceutically acceptable salt thereof substantially free of methanoyl, dehydroxy and 9- keto impurities. Provided also herein are improved and efficient processes for preparing paliperidone intermediates.
    • 本文提供了帕潘立酮,3- [2- [4- [1-(4-呋喃-2-羟基苯基)甲酰基]哌啶基-1-基]乙基] -2-甲基 - 6,7,8,9-四氢-4H-吡啶并[1,2-a]嘧啶-4-酮(甲酰基杂质),3- [2- [4-(6-氟-1,2-苯并异恶唑-3 - 基)-1-哌啶基]乙基] -2-甲基-4H-吡啶并[1,2-a]嘧啶-4-酮(脱羟基杂质)和3- [2- [4-(6-氟-1,2-二氢 - 2-苯并异恶唑-3-基)-1-哌啶基]乙基] -2-甲基-7,8-二氢-6H-吡啶并[1,2-a]嘧啶-4,9-二酮(9-酮杂质), 以及其制备和分离方法。 本文进一步提供基本上不含甲醛酰基,脱羟基和9-酮杂质的高纯度帕潘立酮或其药学上可接受的盐,其制备方法,以及包含基本上不含甲亚酰基的高纯度帕潘立酮或其药学上可接受的盐的药物组合物, 脱羟基和9-酮杂质。 本文还提供了用于制备帕潘立酮中间体的改进且有效的方法。